79207-68-4

Usage

Uses

Used in Pharmaceutical and Agrochemical Industries:
2(1H)-Quinolinone,6-amino-(9CI) is utilized as a precursor in the synthesis of a variety of pharmaceuticals and agrochemicals. Its unique chemical structure allows it to be a key component in the development of new drugs and agricultural products, enhancing their efficacy and performance.
Used in Dye and Pigment Production:
2(1H)-Quinolinone,6-amino-(9CI) also serves as an intermediate in the production of dyes and pigments, contributing to the coloration and stability of various products in the textile, paint, and cosmetic industries.
Used in Research and Development:
2(1H)-Quinolinone,6-amino-(9CI) has been studied for its potential pharmacological properties, including anti-inflammatory and anti-cancer activities. Its exploration in research settings aims to uncover new therapeutic applications and improve existing treatments for various diseases and conditions.

Upstream product

• 64495-55-2 6-nitro-1,2-dihydroquinolin-2-one 
• 613-50-3 6-nitroquinoline 
• 13675-92-8 6-nitroquinoline-N-oxide 
• 64495-55-2 6-nitroquinolin-2-ol 
• 59-31-4 2-quinolone 

Downstream Products

• 569340-07-4 2-oxo-1,2-dihydro-6-quinolinesulfonyl chloride 
• 81839-51-2 6-[4-(3,4-Dimethoxybenzoyl)-1-piperazinyl]-carbostyril 
• 81839-76-1 6-[4-(4-Cyanobenzoyl)-1-piperazinyl]carbostyril 
• 81839-80-7 6-(4-Benzoyl-1-piperazinyl)carbostyril 
• 119924-94-6 3,4-dihydro-6-(1H-imidazol-1-yl)quinolin-2(1H)-one 

Relevant academic research and scientific papers

N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties

Urea transporters (UTs) have been identified as new targets for diuretics. Functional deletion of UTs led to urea-selective urinary concentrating defects with relative salt sparing. In our previous study, a UT inhibitor with a diarylamide scaffold, which is denoted as 11a, was demonstrated as the first orally available UT inhibitor. However, the oral bioavailability of 11a was only 4.38%, which obstructed its clinical application. In this work, by replacing the nitro group of 11a with an acetyl group, 25a was obtained. Compared with 11a, 25a showed a 10 times stronger inhibitory effect on UT-B (0.14 μM vs. 1.41 μM in rats, and 0.48 μM vs. 5.82 μM in mice) and a much higher inhibition rate on UT-A1. Moreover, the metabolic stability both in vitro and in vivo and the drug-like properties (permeability and solubility) of 25a were obviously improved compared with those of 11a. Moreover, the bioavailability of 25a was 15.18%, which was 3 times higher than that of 11a, thereby resulting in significant enhancement of the diuretic activities in rats and mice. 25a showed excellent potential for development as a promising clinical diuretic candidate for targeting UTs to treat diseases that require long-term usage of diuretics, such as hyponatremia.

Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift

Among a series of benzopyridone-based scaffolds investigated as human transient receptor potential vanilloid 1 (TRPV1) ligands, two isomeric benzopyridone scaffolds demonstrated a consistent and distinctive functional profile in which 2-oxo-1,2-dihydroquinolin-5-yl analogues (e.g., 2) displayed high affinity and potent antagonism, whereas 1-oxo-1,2-dihydroisoquinolin-5-yl analogues (e.g., 3) showed full agonism with high potency. Our computational models provide insight into the agonist-antagonist boundary of the analogues suggesting that the Arg557 residue in the S4-S5 linker might be important for sensing the agonist binding and transmitting signals. These results provide structural insights into the TRPV1 and the protein-ligand interactions at a molecular level.

CONDENSED HETEROCYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I) wherein R1, A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

3' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones

A series of selective androgen receptor modulators (SARMs) with a wide spectrum of receptor modulating activities was developed based on optimization of the 4-substituted 6-bisalkylamino-2-quinolinones (3). Significance of the trifluoromethyl group on the side chains and its interactions with amino acid residues within the androgen receptor (AR) ligand binding domain are discussed. A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity.

ENZYME MODULATORS AND TREATMENTS

Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hypervascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein ab1 kinase protein, bcr-ab1 kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.

6-(4-hydroxypiperidino) carboslyril

The present invention is concerned with the compound of formula (I) STR1 and esters and acid addition salts thereof having positive inotrope effect.